(E)-3-(Dimethylamino)-1-(pyrazin-2-YL)prop-2-EN-1-one → 4-((4-(2-(Tert-butoxycarbonylamino)-4-methylthiazol-5-yl)-pyrimidin-2-ylamino)methyl)benzoic acid

HRID 416282

反応式

HRID 416282 の反応式
N1C=CN=CC=1C1C=CN=C([NH:13][CH2:14][C:15]2[CH:23]=[CH:22][C:18]([C:19]([OH:21])=[O:20])=[CH:17][CH:16]=2)N=1.C[N:25](/C=C/C(C1C=NC=CN=1)=O)C.[C:37]([NH:44][C:45]1[S:46][C:47]([C:51](=O)/[CH:52]=[CH:53]/[N:54]([CH3:56])C)=[C:48]([CH3:50])[N:49]=1)([O:39][C:40]([CH3:43])([CH3:42])[CH3:41])=[O:38]>>[C:40]([O:39][C:37]([NH:44][C:45]1[S:46][C:47]([C:51]2[CH:52]=[CH:53][N:54]=[C:56]([NH:13][CH2:14][C:15]3[CH:16]=[CH:17][C:18]([C:19]([OH:21])=[O:20])=[CH:22][CH:23]=3)[N:25]=2)=[C:48]([CH3:50])[N:49]=1)=[O:38])([CH3:41])([CH3:42])[CH3:43]

参加物

4

反応物 3

HCID 5825354(E)-3-(Dimethylamino)-1-(pyrazin-2-YL)prop-2-EN-1-oneHCID 58930506(E)-1-[2-(Boc-Amino-)-4-methylthiazol-5-yl]-3-(dimethylamino)prop-2-en-1-oneHCID 666221674-[(4-Pyrazin-2-yl-pyrimidin-2-ylamino)-methyl]-benzoic acid

生成物 1

HCID 589304744-((4-(2-(Tert-butoxycarbonylamino)-4-methylthiazol-5-yl)-pyrimidin-2-ylamino)methyl)benzoic acid収率 18%

実験手順

Following the procedure described for the synthesis of the acid 25a (scheme 6, step 3) but substituting enamino ketone 23a for the enamino ketone 338, title compound was obtained in 18% yield and was used for the next steps without further purification. MS (m/z): 441.50 (calc) 442.3 (MH+) (found).

出典と根拠

ORDレコード
ord-aeeadea4a66a45d79c56970b509663a4
出典データセット
uspto-grants-2012_01
特許番号
US08088805B2

関連ノート

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